Size | Price | Stock | Qty |
---|---|---|---|
1g |
|
||
2g |
|
||
5g |
|
||
10g |
|
||
25g |
|
||
50g |
|
||
Other Sizes |
|
Purity: ≥98%
Diphenidol HCl (Vontrol; Difenidol), the hydrochloride salt of diphenidol which is an antiemetic, is a potent antagonist of muscarinic M2 and M3 receptors used as an antiemetic and as an antivertigo agent. It inhibits muscarinic M2 and M3 receptors with pKb values of 6.72 and 7.02, respectively. Diphenidol has been approved for the treatment of vomiting and vertigo. Although the mechanism of action of Diphenidol on the vestibular system has not yet been elucidated, it exerts an anticholinergic effect due to interactions with mACh receptors, particularly M1, M2, M3 and M4.
ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Well absorbed from gastrointestinal tract following oral administration. Metabolism / Metabolites IN DOGS & IN MAN, PRINCIPAL URINARY METABOLITE OF DIPHENIDOL...WAS N-(4,4-DIPHENYL-4-HYDROXYBUTYL)-DELTA-AMINOVALERIC ACID...(NOT LESS THAN 50% OF DOSE)... MINOR URINARY METABOLITES INCL A PHENOL...& A LACTAM... Biological Half-Life 4 hours |
---|---|
Toxicity/Toxicokinetics |
Non-Human Toxicity Values
LD50 MICE ORAL 430 MG/KG /HCL/ LD50 MICE INTRAPERITONEAL 105 MG/KG /HCL/ LD50 MICE INTRAVENOUS 37 MG/KG /HCL/ LD50 RATS ORAL 515 MG/KG /HCL/ For more Non-Human Toxicity Values (Complete) data for DIPHENIDOL (6 total), please visit the HSDB record page. |
References |
Neurosci Lett.2015 Mar 4;589:62-6.
|
Additional Infomation |
Diphenidol is a tertiary alcohol that is butan-1-ol substituted by two phenyl groups at position 1 and a piperidin-1-yl group at position 4. It has a role as an antiemetic. It is a member of piperidines, a tertiary alcohol and a member of benzenes.
Diphenidol is an antiemetic agent used in the treatment of vomiting and vertigo. Diphenidol overdose may result in serious toxicity in children. Diphenidol is an Antiemetic. The physiologic effect of diphenidol is by means of Emesis Suppression. Drug Indication For use in the prevention and symptomatic treatment of peripheral (labyrinthine) vertigo and associated nausea and vomiting that occur in such conditions as Meniere's disease and surgery of the middle and inner ear. Also for the control of nausea and vomiting associated with postoperative states, malignant neoplasms, labyrinthine disturbances, antineoplastic agent therapy, radiation sickness, and infectious diseases. FDA Label Mechanism of Action The mechanism by which diphenidol exerts its antiemetic and antivertigo effects is not precisely known. It is thought to diminish vestibular stimulation and depress labyrinthine function and as an antimuscarinic agent. An action on the medullary chemoreceptive trigger zone may also be involved in the antiemetic effect. Diphenidol has no significant sedative, tranquilizing, or antihistaminic action. It has a weak peripheral anticholinergic effect. EXPTL, IT HAS BEEN SHOWN TO EXHIBIT WEAK PARASYMPATHOLYTIC ACTIONS, BUT TO LACK SIGNIFICANT SEDATIVE, TRANQUILIZING, OR ANTIHISTAMINIC PROPERTIES. .../DIPHENIDOL/ IS THOUGHT TO ACT UPON AURAL VESTIBULAR APPARATUS... Therapeutic Uses Antiemetics; Histamine H1 Antagonists ...ANTIEMETIC AGENT FOR ORAL, RECTAL, IM, OR IV ADMIN, USEFUL IN MGMNT OF NAUSEA & VOMITING ASSOC WITH INFECTIOUS DISEASES, MALIGNANCIES, RADIATION SICKNESS, GENERAL ANESTHESIA, TREATMENT WITH ANTINEOPLASTIC AGENTS. ...ALSO USEFUL IN TREATMENT OF VERTIGO OF VESTIBULAR ORIGIN. IN ADULTS, THIS DRUG ALSO IS EFFECTIVE IN...LABYRINTHITIS FOLLOWING SURGERY OF MIDDLE & INNER EAR, & MENIERE'S DISEASE. ITS USE IN TREATMENT OF VERTIGO IN CHILDREN HAS NOT BEEN INVESTIGATED. /HCL/ Drug Warnings SINCE DIPHENIDOL DOES POSSESS PARASYMPATHOLYTIC PROPERITES, IT SHOULD BE USED CAUTIOUSLY IN PT WITH GLAUCOMA, PROSTATIC HYPERTROPHY, PEPTIC ULCER, PYLORIC OR DUODENAL OBSTRUCTION, OR CARDIOSPASM. ...IT IS NOT RECOMMENDED FOR USE IN NAUSEA & VOMITING OF PREGNANCY, SINCE ITS SAFE USE IN THIS CONDITION HAS NOT BEEN ESTABLISHED. Pharmacodynamics Diphenidol is used for control of nausea and vomiting. It has an antivertigo effect on the vestibular apparatus, inhibiting the chemoreceptor trigger zone to control nausea and vomiting, thus preventing motion sickness. |
Molecular Formula |
C21H28CLNO
|
|
---|---|---|
Molecular Weight |
345.91
|
|
Exact Mass |
309.209
|
|
CAS # |
3254-89-5
|
|
Related CAS # |
26363-46-2 (pamoate);3254-89-5 (HCl);972-02-1;
|
|
PubChem CID |
3055
|
|
Appearance |
White to off-white solid powder
|
|
Boiling Point |
473.3ºC at 760 mmHg
|
|
Melting Point |
212-214
104-105 °C |
|
Flash Point |
233.5ºC
|
|
LogP |
4.126
|
|
Hydrogen Bond Donor Count |
1
|
|
Hydrogen Bond Acceptor Count |
2
|
|
Rotatable Bond Count |
6
|
|
Heavy Atom Count |
23
|
|
Complexity |
307
|
|
Defined Atom Stereocenter Count |
0
|
|
InChi Key |
AVZIYZHXZAYGJS-UHFFFAOYSA-N
|
|
InChi Code |
InChI=1S/C21H27NO.ClH/c23-21(19-11-4-1-5-12-19,20-13-6-2-7-14-20)15-10-18-22-16-8-3-9-17-22;/h1-2,4-7,11-14,23H,3,8-10,15-18H2;1H
|
|
Chemical Name |
1,1-Diphenyl-4-piperidin-1-ylbutan-1-ol hydrochloride
|
|
Synonyms |
|
|
HS Tariff Code |
2934.99.9001
|
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
|
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8909 mL | 14.4546 mL | 28.9093 mL | |
5 mM | 0.5782 mL | 2.8909 mL | 5.7819 mL | |
10 mM | 0.2891 mL | 1.4455 mL | 2.8909 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01574313 | Completed | Procedure: stellate ganglion block Drug: 0.25mg, fludiazine Drug: 25mg cephadol@ (diphenidol) Drug: 200mg kentons@ (tocopherol nicotinate). |
Vertigo Meniere Disease |
Chi Mei Medical Hospital | April 2010 | Phase 4 |